Curing the Pains Caused by Forms

It is well known that an API molecule (or drug substance, DS) may exist in various solid forms, including polymorphs, hydrates, solvates, salts, cocrystals and non-crystalline forms. These various solid forms, due to differences in crystal structure, can show significant differences in physicochemical properties that impact the performance of a drug product (DP). Therefore, it is critical to timely identify and select the right form with acceptable solid-state properties, such as crystallinity, hygroscopicity, solubility or dissolution property, stability and processability, for formulation design and regulatory filing.  

To assist drug developers and to stave off issues that can affect the entire development of a drug candidate, we employ an integrated approach to identify the most suitable solid-state form. We conduct effective screening and rigorous assessments for true polymorphs, salts, cocrystals, as well as amorphous solid dispersions (ASDs) of DS, applying comprehensive expertise including:

  • Rational design of form screening using our rich experience based on development phase of a drug candidate; 
  • Intuitive and observative execution of solid form screen and characterization via both simulation and experimental approaches; 
  • In depth understanding of solid-state properties, including crystallinity, hygroscopicity, solubility and/or dissolution, stability and processability for various solid forms; 
  • Skillful investigation of crystal form relationship, determination of relative stability, and expert recommendation of the best solid form for development; 
  • Expert elucidation of single crystal structure for not just filing but fundamental understanding and effective problem solving; 
  • Rich experiences in pre-formulation evaluation, DS crystallization process development, particle engineering and DS-DP co-processing, and DP processing, all facilitates the proper form selection.